Patent NZ-547163-A (NZ)
Title: Derivatives of N-heterocyclylmethylbenzamides, preparation method thereof and application of therapeutics as glycine transport inhibitors
Inventor: DARGAZANLI GIHAD
IPC: A61P25/04
Filed: 2004-10-15
Abstract: Disclosed is a compound corresponding to general formula (I) in which R represents a hydrogen atom or a vinyl group; n represents 0 or 1 or 2 when R represents a hydrogen atom and n represents 1 when R represents a vinyl group; X represents a group of formula CH or a nitrogen atom when R represents a hydrogen atom and X represents a group of formula CH when R represents a vinyl group; R1 represents either a phenyl or naphthyl group optionally substituted with one or more substituents chosen from halogen atoms, linear or branched (C1-C6) alkyl, hydroxyl and (C1-C6)alkoxy groups, the trifluoromethyl group, or a cyclohexyl group, or a heteroaryl group chosen from the thienyl, pyridinyl, oxazolyl, furanyl, thiazolyl, quinolinyl, and isoquinolinyl groups; R2 represents either a hydrogen atom, or one or more substituents chosen from halogen atoms and the trifluoromethyl, (C1-C6) alkyl, (C1-C6) alkoxy, thienyl, phenyloxy, hydroxyl, mercapto, thio (C1-C6) alkyl and cyano groups or a group of general formula -NR4R5 SO2NR4R5, ûSO2 (C1-C6) alkyl, -SO2-phenyl, -CONR4R5 , -COOR7, -CO- (C1-C6) alkyl, -CO-phenyl, -NHCOR8 , -NHSO2- (C1-C6)alkyl, -NHSO2-phenyl and -NHSO2NR4R5 or a group of formula -OCF2O- attached at the 2- and 3-positions of the phenyl group; the groups (C1-C6) alkyl, (C1-C6) alkoxy, -SO2- (C1-C6) alkyl, -CO-(C1-C6)alkyl and -NHSO2-(C1-C6)alkyl being optionally substituted with one or more groups R3; the groups phenyl, -SO2-phenyl, -CO-phenyl and ûNHSO2 phenyl being optionally substituted with a group R6; R3 represents a halogen atom, or a phenyl, (C1-C6) alkoxy or -NR4R5 group; R4 and R5 represent, independently of each other, a hydrogen atom or a (C1-C6) alkyl group or R4 and R5 form with the nitrogen atom bearing them a pyrrolidine ring, a piperidine ring or a morpholine ring; R6 represents a hydrogen atom, a halogen atom, a trifluoromethyl group, a cyano group, a hydroxyl group, a mercapto group, a (C1-C6)alkyl or (C1-C6)alkoxy group; R7 represents a hydrogen atom or a (C1-C6) alkyl group optionally substituted with one or more groups R3, or a phenyl group optionally substituted with a group R6; R8 represents a (C1-C6) alkyl group optionally substituted with one or more groups R3, or a (C1-C6) alkoxy group, or a phenyl group optionally substituted with a group R6, in the form of a free base or of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed is the use of a compound of formula (I) for the preparation of a medicament intended for the treatment of contractures, of pain, of Parkinson's disease and of Parkinsonian symptoms, of epilepsy, of mixed forms and other epileptic syndromes as a supplement to another antiepileptic treatment, or in monotherapy, of sleep apnea, and for neuroprotection. Also disclosed is the use of a compound of formula (I) for the preparation of a medicament intended for the treatment of behavioural disorders associated with dementia, psychoses, various forms of anxiety, panic attacks, phobias, obsessive-compulsive disorders, various forms of depression, of disorders due to alcohol abuse or to withdrawal from alcohol, sexual behaviour disorders, food intake disorders, and migraine.